Jeffery Odell Carter

US Patent:

6413960, Jul 2, 2002

Filed:

May 30, 2000

Appl. No.:

09/609011

Inventors:

John J Talley - St. Louis MO
Thomas D Penning - Elmhurst IL
Paul W Collins - Deerfield IL
James W Malecha - Libertyville IL
Julie M Miyashiro - Chicago IL
Stephen R Bertenshaw - Brentwood MO
Ish K Khanna - Vernon Hills IL
Matthew J Graneto - St. Louis MO
Roland S Rogers - Richmond Heights MO
Jeffery S Carter - Chesterfield MO
Stephen H. Docter - Mt. Prospect IL
Stella S Yu - Morton Grove IL

Assignee:

G.D. Searle Co. - Chicago IL

International Classification:

A61P 1106

US Classification:

5142365, 514406

Abstract:

A class of pyrazolyl benzenesulfonamide compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II: wherein R is selected from hydrido, alkyl, haloalkyl, alkoxycarbonyl, cyano, cyanoalkyl, carboxyl, aminocarbonyl, alkylaminocarbonyl, cycloalkylaminocarbonyl, arylaminocarbonyl, carboxyalkylaminocarbonyl, carboxyalkyl, aralkoxycarbonylalkylaminocarbonyl, aminocarbonylalkyl, alkoxycarbonylcyanoalkenyl and hydroxyalkyl; wherein R is selected from hydrido, alkyl, cyano, hydroxyalkyl, cycloalkyl, alkylsulfonyl and halo; and wherein R is selected from aralkenyl, aryl, cycloalkyl, cycloalkenyl and heterocyclic; wherein R is optionally substituted at a substitutable position with one or more radicals selected from halo, alkylthio, alkylsulfonyl, cyano, nitro, haloalkyl, alkyl, hydroxyl, alkenyl, hydroxyalkyl, carboxyl, cycloalkyl, alkylamino, dialkylamino, alkoxycarbonyl, aminocarbonyl, alkoxy, haloalkoxy, sulfamyl, heterocyclic and amino; provided R and R are not both hydrido; further provided that R is not carboxyl or methyl when R is hydrido and when R is phenyl; further provided that R is not triazolyl when R is methyl; further provided that R is not aralkenyl when R is carboxyl, aminocarbonyl or ethoxycarbonyl; further provided that R is not phenyl when R is methyl and R is carboxyl; and further provided that R is not unsubstituted thienyl when R is trifluoromethyl; or a pharmaceutically-acceptable salt thereof.

US Patent:

6436967, Aug 20, 2002

Filed:

Sep 14, 2000

Appl. No.:

09/661859

Inventors:

John J Talley - St. Louis MO
James W Malecha - Libertyville IL
Stephen Bertenshaw - Cheshire CT
Matthew J Graneto - Chesterfield MO
Jeffery Carter - Chesterfield MO
Jinglin Li - Hopewell NJ
Srinivasan Nagarajan - Chesterfield MO
David L Brown - Chesterfield MO
Thomas D Penning - Elmhurst IL
Ish K Khanna - Vernon Hills IL
Xiangdong Xu - Gurnee IL
Richard M Weier - Lake Bluff IL

Assignee:

Pharmacia Corporation - St. Louis MO

International Classification:

A61K 3144

US Classification:

514341, 514377, 514399, 514400, 514403, 514406, 514602, 5462741, 546290, 548225, 548228, 548229, 548235, 5483147, 5483151, 5483154, 5483355, 5483385, 5483595, 5483751, 5483761, 5483771, 548549, 548556, 564 84, 564 91

Abstract:

This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to prodrugs of compounds which selectively inhibit cyclooxygenase-2. The use of non-steroidal antiinflammatory drugs (NSAIDs) in treating pain and the swelling associated with inflammation also produce severe side effects, including life threatening ulcers. The recent discovery of an inducible enzyme associated with inflammation (âprostaglandin G/H synthase IIâ or âcyclooxygenase-2 (COX-2)â) provides a viable target of inhibition which more effectively reduces inflammation and produces fewer and less drastic side effects.

US Patent:

6492411, Dec 10, 2002

Filed:

Apr 17, 2002

Appl. No.:

10/125325

Inventors:

John J Talley - St. Louis MO
Thomas D Penning - Elmhurst IL
Paul W Collins - Deerfield IL
James W Malecha - Libertyville IL
Julie M Miyashiro - Chicago IL
Stephen R Bertenshaw - Brentwood MO
Ish K Khanna - Vernon Hills IL
Matthew J Graneto - St. Louis MO
Roland S Rogers - Richmond Heights MO
Jeffery S Carter - Chesterfield MO
Stephen H. Docter - Mt. Prospect IL
Stella S Yu - Morton Grove IL

Assignee:

G. D. Searle Co. - Chicago IL

International Classification:

A61P 2900

US Classification:

514406, 5142365

Abstract:

A class of pyrazolyl benzenesulfonamide compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II: wherein R is selected from hydrido, alkyl, haloalkyl, alkoxycarbonyl, cyano, cyanoalkyl, carboxyl, aminocarbonyl, alkylaminocarbonyl, cycloalkylaminocarbonyl, arylaminocarbonyl, carboxyalkylaminocarbonyl, carboxyalkyl, aralkoxycarbonylalkylaminocarbonyl, aminocarbonylalkyl, alkoxycarbonylcyanoalkenyl and hydroxyalkyl; wherein R is selected from hydrido, alkyl, cyano, hydroxyalkyl, cycloalkyl, alkylsulfonyl and halo; and wherein R is selected from aralkenyl, aryl, cycloalkyl, cycloalkenyl and heterocyclic; wherein R is optionally substituted at a substitutable position with one or more radicals selected from halo, alkylthio, alkylsulfonyl, cyano, nitro, haloalkyl, alkyl, hydroxyl, alkenyl, hydroxyalkyl, carboxyl, cycloalkyl, alkylamino, dialkylamino, alkoxycarbonyl, aminocarbonyl, alkoxy, haloalkoxy, sulfamyl, heterocyclic and amino; provided R and R are not both hydrido; further provided that R is not carboxyl or methyl when R is hydrido and when R is phenyl; further provided that R is not triazolyl when R is methyl; further provided that R is not aralkenyl when R is carboxyl, aminocarbonyl or ethoxycarbonyl; further provided that R is not phenyl when R is methyl and R is carboxyl; and further provided that R is not unsubstituted thienyl when R is trifluoromethyl; or a pharmaceutically-acceptable salt thereof.

US Patent:

6586603, Jul 1, 2003

Filed:

Oct 21, 2002

Appl. No.:

10/274679

Inventors:

John J Talley - St. Louis MO
Thomas D Penning - Elmhurst IL
Paul W Collins - Deerfield IL
James W Malecha - Libertyville IL
Julie M Miyashiro - Chicago IL
Stephen R. Bertenshaw - Brentwood MO
Ish K Khanna - Vernon Hills IL
Matthew J Graneto - St. Louis MO
Roland S Rogers - Richmond Heights MO
Jeffery S Carter - Chesterfield MO
Stephen H Docter - Mt. Prospect IL
Stella S Yu - Morton Grove IL

Assignee:

G.D. Searle Co. - Chicago IL

International Classification:

C07D23112

US Classification:

5483771

Abstract:

A class of pyrazolyl benzenesulfonamide compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II: wherein R is selected from hydrido, alkyl, haloalkyl, alkoxycarbonyl, cyano, cyanoalkyl, carboxyl, aminocarbonyl, alkylaminocarbonyl, cycloalkylaminocarbonyl, arylaminocarbonyl, carboxyalkylaminocarbonyl, carboxyalkyl, aralkoxycarbonylalkylaminocarbonyl, aminocarbonylalkyl, alkoxycarbonylcyanoalkenyl and hydroxyalkyl; wherein R is selected from hydrido, alkyl, cyano, hydroxyalkyl, cycloalkyl, alkylsulfonyl and halo; and wherein R is selected from aralkenyl, aryl, cycloalkyl, cycloalkenyl and heterocyclic; wherein R is optionally substituted at a substitutable position with one or more radicals selected from halo, alkylthio, alkylsulfonyl, cyano, nitro, haloalkyl, alkyl, hydroxyl, alkenyl, hydroxyalkyl, carboxyl, cycloalkyl, alkylamino, dialkylamino, alkoxycarbonyl, aminocarbonyl, alkoxy, haloalkoxy, sulfamyl, heterocyclic and amino; provided R and R are not both hydrido; further provided that R is not carboxyl or methyl when R is hydrido and when R is phenyl; further provided that R is not triazolyl when R is methyl; further provided that R is not aralkenyl when R is carboxyl, aminocarbonyl or ethoxycarbonyl; further provided that R is not phenyl when R is methyl and R is carboxyl; and further provided that R is not unsubstituted thienyl when R is trifluoromethyl; or a pharmaceutically-acceptable salt thereof.

US Patent:

6716991, Apr 6, 2004

Filed:

Mar 4, 2003

Appl. No.:

10/378781

Inventors:

John J Talley - St Louis MO
Thomas D Penning - Elmhurst IL
Paul W Collins - Deerfield IL
James W Malecha - Libertyville IL
Julie M Miyashiro - Chicago IL
Stephen R Bertenshaw - Brentwood MO
Ish K Khanna - Vernon Hills IL
Matthew J Graneto - St. Louis MO
Roland S Rogers - Richmond Heights MO
Jeffery S Carter - Chesterfield MO
Stephen H. Doctor - Mt. Prospect IL
Stella S Yu - Morton Grove IL

Assignee:

G. D. Searle Co. - Chicago IL

International Classification:

C07D23112

US Classification:

5483771

Abstract:

A class of pyrazolyl benzenesulfonamide compounds is descrbed for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II: wherein R is selected from hydrido, alkyl, haloalkyl, alkoxycarbonyl, cyano, cyanoalkyl, carboxyl, aminocarbonyl, alkylaminocarbonyl, cycloalkylaminocarbonyl, arylaminocarbonyl, carboxyalkylaminocarbonyl, carboxyalkyl, aralkoxycarbonylalkylaminocarbonyl, aminocarbonylalkyl, alkoxycarbonylcyanoalkenyl and hydroxyalkyl; wherein R is selected from hydrido, alkyl, cyano, hydroxyalkyl, cycloalkyl, alkylsulforyl and halo; and wherein R is selected from aralkenyl, aryl, cycloalkyl, cycloalkenyl and heterocyclic; wherein R is optionally substituted at a substitutable position with one or more radicals selected from halo, alkylthio, alkylsulfonyl, cyano, nitro, haloalkyl, alkyl, hydroxyl, alkenyl, hydroxyalkyl, carboxy, cycloalkyl, alkylamino, dialkylamino, alkoxycarbonyl, aminocarbonyl, alkoxy, haloalkoxy, sulfamyl, heterocyclic and amino; provided R and R are not both hydrido; further provided that R is not carboxyl or methyl when R is hydrido and when R is phenyl; further provided that R is not triazolyl when R is methyl; further provided that R is not aralkenyl when R is carboxyl, aminocarbonyl or ethoxycarbonyl; further provided that R is not phenyl when R is methyl and R is carboxyl; and further provided that R is not unsubstituted thienyl when R is trifluoromethyl; or a pharmceutically-acceptable salt thereof.

US Patent:

6951949, Oct 4, 2005

Filed:

Nov 3, 2003

Appl. No.:

10/700019

Inventors:

John J Talley - St. Louis MO, US
Thomas D Penning - Elmhurst IL, US
Paul W Collins - Deerfield IL, US
James W Malecha - Libertyville IL, US
Julie M Miyashiro - Chicago IL, US
Stephen R Bertenshaw - Brentwood MO, US
Ish K Khanna - Vernon Hills IL, US
Matthew J Graneto - St. Louis MO, US
Roland S Rogers - Richmond Heights MO, US
Jeffery S Carter - Chesterfield MO, US
Stephen H. Docter - Mt. Prospect IL, US
Stella S Yu - Morton Grove IL, US

Assignee:

Pharmacia Corporation - St. Louis MO

International Classification:

C07D231/12

US Classification:

5483771

Abstract:

A class of pyrazolyl benzenesulfonamide compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II: wherein Ris selected from hydrido, alkyl, haloalkyl, alkoxycaronyl, cyano, cyanoalkyl, carboxyl, aminocaronyl, alkylaminocarbonyl, cycloalklaminocarbonyl, arylaminocarbonyl, carboxyalkylaminocarbonyl, carboxyalkyl, aralkoxycarbonylalkylaminocarbonyl, amioncarbonylalkyl, alkoxycarbonylcyanoalkenyl and hydroxyalkyl; wherein Ris selected from hydrido, alkyl, cyano, hydroxyalkyl, cycloalkyl, alkylsulfonyl and halo; and wherein Ris selected from aralkenyl, aryl, cycloalkyl, cycloalkenyl and heterocyclic; wherein Ris optionally substituted at a substitutable position with one or more radicals selected from halo alkylthio, alkylsulfonyl, cyano, nitro, haloalkyl, alkyl, hydroxyl, alkenyl, hydroxyalkyl, carboxyl, cycloalkyl, alkylamino, dialkylamino, alkoxycarbonyl, aminocarbonyl, alkoxy, haloalkoxy, sulfamyl, heterocyclic and amino; provided Rand Rare not both hydrido; further provided that Ris not carboxyl or methyl when Ris hydrido and when Ris phenyl; further provided that Ris not triazolyl when Ris methyl; further provided that Ris not arakenyl when Ris carboxyl, aminocarbonyl or ethoxycarbonyl; further provided that Ris not phenyl when Ris methyl and Ris carboxyl; and further provided that Ris not unsubstituted thienyl when Ris trifluoromethyl; or a pharmaceutically-acceptable salt thereof.

US Patent:

20050131050, Jun 16, 2005

Filed:

Jan 31, 2005

Appl. No.:

11/048037

Inventors:

John Talley - St. Louis MO, US
Thomas Penning - Elmhurst IL, US
Paul Collins - Deerfield IL, US
Donald Rogier - St. Louis MO, US
James Malecha - Libertyville IL, US
Julie Miyashiro - Chicago IL, US
Stephen Bertenshaw - Brentwood MO, US
Ish Khanna - Vernon Hills IL, US
Matthew Graneto - St. Louis MO, US
Roland Rogers - Richmond Heights MO, US
Jeffery Carter - Chesterfield MO, US
Stephen Docter - Mt. Prospect IL, US
Stella Yu - Morton Grove IL, US

Assignee:

G.D. Searle & Co. - chicago IL

International Classification:

A61K031/416
A61K031/4152
C07D045/02
C07D231/10

US Classification:

514406000, 548364400, 548371100

Abstract:

A class of pyrazolyl benzenesulfonamide compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II: wherein Ris selected from hydrido, alkyl, haloalkyl, alkoxycaronyl, cyano, cyanoalkyl, carboxyl, aminocaronyl, alkylaminocarbonyl, cycloalklaminocarbonyl, arylaminocarbonyl, carboxyalkylaminocarbonyl, carboxyalkyl, aralkoxycarbonylalkylaminocarbonyl, amioncarbonylalkyl, alkoxycarbonylcyanoalkenyl and hydroxyalkyl; wherein Ris selected from hydrido, alkyl, cyano, hydroxyalkyl, cycloalkyl, alkylsulfonyl and halo; and wherein Ris selected from aralkenyl, aryl, cycloalkyl, cycloalkenyl and heterocyclic; wherein Ris optionally substituted at a substitutable position with one or more radicals selected from halo alkylthio, alkylsulfonyl, cyano, nitro, haloalkyl, alkyl, hydroxyl, alkenyl, hydroxyalkyl, carboxyl, cycloalkyl, alkylamino, dialkylamino, alkoxycarbonyl, aminocarbonyl, alkoxy, haloalkoxy, sulfamyl, heterocyclic and amino; provided Rand Rare not both hydrido; further provided that Ris not carboxyl or methyl when Ris hydrido and when Ris phenyl; further provided that Ris not triazolyl when Ris methyl; further provided that Ris not arakenyl when Ris carboxyl, aminocarbonyl or ethoxycarbonyl; further provided that Ris not phenyl when Ris methyl and Ris carboxyl; and further provided that Ris not unsubstituted thienyl when Ris trifluoromethyl; or a pharmaceutically-acceptable salt thereof.

US Patent:

55084265, Apr 16, 1996

Filed:

Jun 1, 1995

Appl. No.:

8/457185

Inventors:

John J. Talley - St. Louis MO
Thomas D. Penning - Elmhurst IL
Paul W. Collins - Deerfield IL
Donald J. Rogier - St. Louis MO
James W. Malecha - Libertyville IL
Julie M. Miyashiro - Chicago IL
Stephen R. Bertenshaw - Brentwood MO
Ish K. Khanna - Vernon Hills IL
Matthew J. Graneto - St. Louis MO
Roland S. Rogers - Richmond Heights MO
Jeffery S. Carter - Chesterfield MO

Assignee:

G. D. Searle & Co. - Skokie IL

International Classification:

C07D23154

US Classification:

5483591

Abstract:

A class of pyrazolyl benzenesulfonamide compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I: ##STR1## or a pharmaceutically-acceptable salt thereof.